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CYP3A4-IN-1

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16

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150574
    CYP3A4-IN-1

    		Cytochrome P450 Infection
    CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC50 value of 0.085 µM .
    CYP3A4-IN-1
  • HY-N8354
    6',7'-Dihydroxybergamottin

    6′,7′-DHB

    		 Cytochrome P450 Cardiovascular Disease
    6',7'-Dihydroxybergamottin (6′,7′-DHB), a furanocoumarin, is a potent CYP3A4 inhibitor .
    6',7'-Dihydroxybergamottin
  • HY-B1012
    Quinestrol

    W-3566

    		 Estrogen Receptor/ERR Cytochrome P450 GnRH Receptor Metabolic Disease Endocrinology
    Quinestrol (W-3566) is an orally effective synthetic estrogen compound that acts on CYP3A4, CYP1A2, and GnRH. Quinestrol interferes with GnRH release and disrupts the hypothalamic-pituitary-ovarian axis. Quinestrol downregulates the gene expression of follicle-stimulating hormone β and luteinizing hormone β, induces oxidative stress, damages reproductive organs, reduces sperm density and motility, increases sperm malformation rate, and alters the levels of sex hormones such as testosterone, luteinizing hormone, estradiol, and progesterone. Quinestrol can be used in studies related to reproductive function regulation .
    Quinestrol
  • HY-14362
    GSK-25

    		ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
    GSK-25
  • HY-121580
    Tabimorelin

    NN703

    		 Cytochrome P450 Endocrinology
    Tabimorelin (NN703) is an orally active growth hormone (GH) secretagogue. Tabimorelin is also a potent inhibitor of CYP3A4 activity .
    Tabimorelin
  • HY-16785B
    Veledimex (S enantiomer)

    INXN-1001 (S enantiomer); RG-115932 (S enantiomer)

    		 Interleukin Related Cancer
    Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5 .
    Veledimex (S enantiomer)
  • HY-107461
    LY2623091

    		Glucocorticoid Receptor Cardiovascular Disease
    LY2623091 is a mineralocorticoid receptor antagonist for the treatment of refractory hypertension. LY2623091 exhibits CYP3A4-dependent clearance and synergistic effects with CYP3A4 inhibitors .
    LY2623091
  • HY-146177
    CYP3A4 enzyme-IN-1

    		Bacterial Cytochrome P450 Infection
    CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
    CYP3A4 enzyme-IN-1
  • HY-103540
    Tabimorelin hemifumarate

    NN703 hemifumarate

    		 Cytochrome P450 Endocrinology
    Tabimorelin (NN703) hemifumarate is an orally active growth hormone (GH) secretagogue. Tabimorelin hemifumarate is also a potent inhibitor of CYP3A4 activity .
    Tabimorelin hemifumarate
  • HY-156330
    HIV-IN-9

    		HIV Cytochrome P450 Infection
    HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
    HIV-IN-9
  • HY-149813
    P-gp inhibitor 14

    		P-glycoprotein Cancer
    P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity .
    P-gp inhibitor 14
  • HY-147999
    GlcN-6-P Synthase-IN-1

    		Bacterial Fungal Cytochrome P450 Infection
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
    GlcN-6-P Synthase-IN-1
  • HY-148597
    FGFR-IN-10

    		FGFR Cytochrome P450 Cancer
    FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .
    FGFR-IN-10
  • HY-172393
    TCF4/β-catenin-IN-1

    		β-catenin Apoptosis Caspase MDM-2/p53 Bcl-2 Family Cytochrome P450 Cancer
    TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells .
    TCF4/β-catenin-IN-1
  • HY-175804
    M2 ion channel blocker-2

    		SARS-CoV Infection
    M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC50: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .
    M2 ion channel blocker-2
  • HY-B1012R
    Quinestrol (Standard)

    W-3566 (Standard)

    		 Reference Standards Estrogen Receptor/ERR Metabolic Disease Endocrinology
    Quinestrol (Standard) is the analytical standard of Quinestrol (HY-B1012). This product is intended for research and analytical applications. Quinestrol (W-3566) is an orally effective synthetic estrogen compound that acts on CYP3A4, CYP1A2, and GnRH. Quinestrol interferes with GnRH release and disrupts the hypothalamic-pituitary-ovarian axis. Quinestrol downregulates the gene expression of follicle-stimulating hormone β and luteinizing hormone β, induces oxidative stress, damages reproductive organs, reduces sperm density and motility, increases sperm malformation rate, and alters the levels of sex hormones such as testosterone, luteinizing hormone, estradiol, and progesterone. Quinestrol can be used in studies related to reproductive function regulation .
    Quinestrol (Standard)

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